4-(呋喃-2-基)-2-甲基-5-氧代-N-(邻甲苯基)-1,4,5,6,7,8-六氢喹啉-3-甲酰胺

• 常用名: 4-(呋喃-2-基)-2-甲基-5-氧代-N-(邻甲苯基)-1,4,5,6,7,8-六氢喹啉-3-甲酰胺
• 英文名: FFA3 agonist 1
• CAS号: 886358-51-6
• 分子量: 362.42
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₂H₂₂N₂O₃
• 熔点: N/A
• 闪点: N/A

用途

FFA3激动剂1(化合物24)是游离脂肪酸受体3(FFA3)的激动剂。FFA3激动剂1通过激活FFA3调节肠道微生物群的健康效应[1]。

名称

• 中文名: 4-(呋喃-2-基)-2-甲基-5-氧代-N-(邻甲苯基)-1,4,5,6,7,8-六氢喹啉-3-甲酰胺
• 英文名: 4-(Furan-2-yl)-2-methyl-5-oxo-N-(o-tolyl)-1,4,5,6,7,8-hexahydroquinoline-3-carboxamide

生物活性

• 描述: FFA3激动剂1(化合物24)是游离脂肪酸受体3(FFA3)的激动剂。FFA3激动剂1通过激活FFA3调节肠道微生物群的健康效应[1]。
• 相关类别:
  研究领域 >> 炎症/免疫
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> GPR40
  研究领域 >> 代谢疾病
• 体外研究: FFA3激动剂1增加诱导表达增强黄色荧光蛋白 (eYFP)人游离脂肪酸受体 3(hFFA3)的 螺纹内螺纹REx 293细胞中的 [35S]GTPgS公司的掺入和 pERK1/2型的产生,减少中 营地的产生[2]。 FFA3激动剂1增加人游离脂肪酸受体 3.鼠游离脂肪酸受体 3(mFFA3)、兔游离脂肪酸受体 3(rFFA3)中 [35S]GTPgS公司的掺入[2]。
• 参考文献:

  [1]. Ulven ER, et al. Structure-Activity Relationship Studies of Tetrahydroquinolone Free Fatty Acid Receptor 3 Modulators. J Med Chem. 2020 Apr 9;63(7):3577-3595.

  [2]. Hudson BD, Christiansen E, Murdoch H, Jenkins L, Hansen AH, Madsen O, Ulven T, Milligan G. Complex pharmacology of novel allosteric free fatty acid 3 receptor ligands. Mol Pharmacol. 2014 Aug;86(2):200-10.

物理化学性质

• 分子式: C₂₂H₂₂N₂O₃
• 分子量: 362.42
• InChIKey: HIWQJAGWEWRIIP-UHFFFAOYSA-N
• SMILES: CC1=C(C(=O)Nc2ccccc2C)C(c2ccco2)C2=C(CCCC2=O)N1

靶点实验

查看更多实验

实验名称：Agonist activity at human C-terminal eYFP tagged FFA1 receptor stably expressed in HE... 来源：ChEMBL 靶标：Free fatty acid receptor 1 External Id：CHEMBL4404878

实验名称：Agonist activity at human C-terminal eYFP tagged FFA4 receptor stably expressed in HE... 来源：ChEMBL 靶标：Free fatty acid receptor 4 External Id：CHEMBL4404879

实验名称：Agonist activity at human C-terminal eYFP tagged FFA2 receptor stably expressed in Fl... 来源：ChEMBL 靶标：Free fatty acid receptor 2 External Id：CHEMBL4404880

实验名称：Agonist activity at human C-terminal Gia tagged GPR84 receptor stably expressed in Fl... 来源：ChEMBL 靶标：G-protein coupled receptor 84 External Id：CHEMBL4404881

实验名称：Displacement of [3H]-PN200-110 from recombinant full length human L-type calcium chan... 来源：ChEMBL 靶标：Voltage-dependent L-type calcium channel subunit alpha-1C External Id：CHEMBL4404882

实验名称：Volume of distribution in BALB/c mouse at 5 mg/kg, iv measured up to 1440 mins by HPL... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4404869

实验名称：Total clearance in BALB/c mouse at 5 mg/kg, iv measured up to 1440 mins by HPLC-MS/MS... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4404870

实验名称：Half life in BALB/c mouse at 10 mg/kg, po measured up to 1440 mins by HPLC-MS/MS anal... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4404871

实验名称：Tmax in BALB/c mouse at 10 mg/kg, po measured up to 1440 mins by HPLC-MS/MS analysis 来源：ChEMBL 靶标：N/A External Id：CHEMBL4404872

实验名称：AUC infinity in BALB/c mouse at 10 mg/kg, po measured up to 1440 mins by HPLC-MS/MS a... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4404874

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